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公开(公告)号：EP4374924A3
公开(公告)日：2024-08-07
申请号：EP24154479.0
申请日：2014-10-17
Applicant: Novartis AG
Inventor： EDER, Matthias , KOPKA, Klaus , SCHÄFER, Martin , BAUDER-WÜST, Ulrike , HABERKORN, Uwe , BENESOVA, Martina , MIER, Walter , KLIEM, Hans-Christian , KRATOCHWIL, Clemens , EISENHUT, Michael
IPC: C07D295/145 , C07B59/00 , A61K51/04 , A61P35/00 , C07D257/02 , A61P35/04 , A61P13/08
CPC classification number: C07B59/002 , C07D295/145 , A61K51/0402 , A61K51/0497 , C07D257/02 , A61P13/08 , A61P35/00 , A61P35/04
Abstract: The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer.
Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).
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公开(公告)号：EP4008715A1
公开(公告)日：2022-06-08
申请号：EP19940643.0
申请日：2019-12-20
Applicant: Suqian Keylab Biochemical Co., Ltd.
Inventor： WANG, Mingchun , LI, Qingyi
IPC: C07D295/104 , C07D295/145 , C07D231/14 , A01N43/56 , A01P3/00
Abstract: The present invention relates to a preparation method for a halogen-substituted compound, where a piperazine derivative shown in formula I reacts with a halogenated acetyl halide derivative shown in formula VI to generate a halogen-substituted compound shown in formula II. The present invention further relates to a preparation method for preparing a pyrazole derivative by using a halogen-substituted compound, where a halogen-substituted compound shown in formula II reacts with methylhydrazine to close a pyrazole ring, to generate a halogen-substituted alkyl-1-methylpyrazole derivative shown in formula IV, or reacts with methylhydrazine benzaldehyde hydrazone to generate a hydrazone compound shown in formula III, which closes, under the action of an acid, a pyrazole ring to generate a halogen-substituted alkyl-1-methylpyrazole derivative shown in formula IV The present invention further relates to a structure of an intermediate compound. The preparation methods for a halogen-substituted compound and a pyrazole derivative of the present invention are suitable for industrial production.
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公开(公告)号：EP3853213A1
公开(公告)日：2021-07-28
申请号：EP19863710.0
申请日：2019-09-19
Applicant: Endocyte, Inc.
Inventor： LEAMON, Christopher, Paul , VLAHOV, Iontcho, Radoslavov
IPC: C07D295/145 , C07F9/38 , C07F9/40
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4.发明公开Labeled inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer 审中-公开前列腺特异性膜抗原的经标记的抑制剂（PSMA），它们作为显像剂和药物组合物中用于前列腺癌的治疗
公开(公告)号：EP2862857A1
公开(公告)日：2015-04-22
申请号：EP13004991.9
申请日：2013-10-18
Inventor： Eder, Matthias , Kopka, Klaus , Schäfer, Martin , Bauder-Wüst, Ulrike , Haberkorn, Uwe , Eisenhut, Michael, Prof. , Mier, Walter, Dr. , Benesova, Martina
IPC: C07D295/145 , C07B59/00 , A61K51/04 , A61P35/00
CPC classification number: C07D295/145 , C07B59/002
Abstract: The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer.
Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).Abstract translation: 本发明基因集会涉及到放射性药物领域及其核医学作为示踪剂，造影剂的使用和前列腺癌的各种疾病状态的治疗。 因此，本发明涉及的化合物也由通式（Ia）或（Ib）表示。
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公开(公告)号：EP2513057A1
公开(公告)日：2012-10-24
申请号：EP10782202.5
申请日：2010-11-22
Applicant: Merck Patent GmbH
Inventor： STIEBER, Frank , WIENKE, Dirk
IPC: C07D213/63 , C07D239/42 , C07D251/40 , C07D401/14 , C07D403/04 , C07D295/145 , A61K31/4427 , A61K31/506 , A61K31/53 , A61P35/00 , A61P29/00
CPC classification number: C07D295/088 , A61K31/444 , C07B2200/05 , C07D213/61 , C07D213/65 , C07D213/74 , C07D239/42 , C07D241/20 , C07D251/22 , C07D295/033 , C07D295/096 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/14 , C07F5/025
Abstract: The present invention relates to compounds of the formula (I), where R
1 , R
2 , R
3 , R
4 , R
5 , R
6 , R
7 , R
8 , R
9 , R
10 , R
11 , R
12 , R
13 , R
14 , R
15 , R
16 , R
17 , M
1, M
2 , M
3 , M
4 , Y
1 , Y
2 , V, W, n, m and o have the meaning specified in claim 1, and to physiologically compatible salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases that are influenced by inhibiting sphingosine kinase 1.
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6.发明授权VERFAHREN ZUR HERSTELLUNG HALOGENSUBSTITUIERTER 2-(AMINOMETHYLIDEN)-3-OXOBUTTERSÄUREESTER 有权用于生产方法卤素取代的2-（氨基亚甲基）-3-氧代丁酸
公开(公告)号：EP2297111B1
公开(公告)日：2012-06-20
申请号：EP09738223.8
申请日：2009-04-30
Applicant: BASF SE
Inventor： ZIERKE, Thomas , MAYWALD, Volker , RACK, Michael , SMIDT, Sebastian Peer , KEIL, Michael , WOLF, Bernd , KORADIN, Christopher
IPC: C07D231/14 , C07D295/145
CPC classification number: C07D295/145 , C07D231/14
Abstract: The present invention relates to a method for producing 2- (aminomethylidene)-4,4dihalo-3-oxobutyric acid esters of the formula (I), where R
1 , R
2 , R
3 are C
1 -C
6 -alkyl, C
1 -C
6 -haloalkyl, C
2 -C
6 -alkenyl, C
3 -C
10 -cycloalkyl or benzyl and/or R
2 together with R
3 and the nitrogen atom, to which both radicals are bound, are a heterocyclic radical, wherein a corresponding 3-aminoacrylic acid ester is reacted with a halogen-substituted acetyl fluoride in the presence of at least one alkali or earth alkali metal fluoride. The invention also relates to the further reaction of halogen-substituted 2-(aminomethylidene)-3-oxobutyric acid esters of the formula (1) into halomethyl-substituted pyrazole-4-ylcarboxylic acids and the esters thereof.
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7.发明授权NITRO-SUBSTITUTED PHENYL-PIPERAZINE COMPOUNDS, THEIR PREPARATION AND USE IN MEDICAMENTS 有权硝基取代的苯基PHENYLPIPERAZINVERBINDUNGEN，生产和它们在药物
公开(公告)号：EP1851210B1
公开(公告)日：2011-10-19
申请号：EP05824122.5
申请日：2005-12-29
Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
Inventor： ASCHENBRENNER, Andrea , KRAUS, Jürgen , TASLER, Stefan , WUZIK, Andreas , QUINTANA-RUIZ, Jordi-Ramon
IPC: C07D295/145 , C07D295/096 , C07D207/50 , C07D207/335 , C07D213/74 , C07D231/12 , C07D237/14 , A61K31/495 , A61K31/496 , A61P25/24 , C07D271/12
CPC classification number: C07D207/325 , C07D207/50 , C07D213/74 , C07D295/096 , C07D295/135
Abstract: The present invention relates to nitro-substituted phenyl-piperazine compounds of general formula I, a process for their preparation, medicaments comprising said nitro-substituted phenyl-piperazine compounds as well as the use of said nitro-substituted phenylpiperazine compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.
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8.发明公开VERFAHREN ZUR HERSTELLUNG HALOGENSUBSTITUIERTER 2-(AMINOMETHYLIDEN)-3-OXOBUTTERSÄUREESTER 有权用于生产方法卤素取代的2-（氨基亚甲基）-3-氧代丁酸
公开(公告)号：EP2297111A2
公开(公告)日：2011-03-23
申请号：EP09738223.8
申请日：2009-04-30
Applicant: BASF SE
Inventor： ZIERKE, Thomas , MAYWALD, Volker , RACK, Michael , SMIDT, Sebastian Peer , KEIL, Michael , WOLF, Bernd , KORADIN, Christopher
IPC: C07D231/14 , C07D295/145
CPC classification number: C07D295/145 , C07D231/14
Abstract: The present invention relates to a method for producing 2- (aminomethylidene)-4,4dihalo-3-oxobutyric acid esters of the formula (I), where R
1 , R
2 , R
3 are C
1 -C
6 -alkyl, C
1 -C
6 -haloalkyl, C
2 -C
6 -alkenyl, C
3 -C
10 -cycloalkyl or benzyl and/or R
2 together with R
3 and the nitrogen atom, to which both radicals are bound, are a heterocyclic radical, wherein a corresponding 3-aminoacrylic acid ester is reacted with a halogen-substituted acetyl fluoride in the presence of at least one alkali or earth alkali metal fluoride. The invention also relates to the further reaction of halogen-substituted 2-(aminomethylidene)-3-oxobutyric acid esters of the formula (1) into halomethyl-substituted pyrazole-4-ylcarboxylic acids and the esters thereof.
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9.发明公开NITRO-SUBSTITUTED PHENYL-PIPERAZINE COMPOUNDS, THEIR PREPARATION AND USE IN MEDICAMENTS 有权硝基取代的苯基PHENYLPIPERAZINVERBINDUNGEN，生产和它们在药物
公开(公告)号：EP1851210A2
公开(公告)日：2007-11-07
申请号：EP05824122.5
申请日：2005-12-29
Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
Inventor： ASCHENBRENNER, Andrea , KRAUS, Jürgen , TASLER, Stefan , WUZIK, Andreas , QUINTANA-RUIZ, Jordi-Ramon
IPC: C07D295/145 , C07D295/096 , C07D207/50 , C07D207/335 , C07D213/74 , C07D231/12 , C07D237/14 , A61K31/495 , A61K31/496 , A61P25/24 , C07D271/12
CPC classification number: C07D207/325 , C07D207/50 , C07D213/74 , C07D295/096 , C07D295/135
Abstract: The present invention relates to nitro-substituted phenyl-piperazine compounds of general formula I, a process for their preparation, medicaments comprising said nitro-substituted phenyl-piperazine compounds as well as the use of said nitro-substituted phenylpiperazine compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.
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公开(公告)号：EP0731797B1
公开(公告)日：1999-09-08
申请号：EP95901433.3
申请日：1994-11-25
Applicant: BRACCO S.p.A. , DIBRA S.p.A.
Inventor： FELDER, Ernst , ANELLI, Pier, Lucio , VIRTUANI, Mario , BELTRAMI, Andrea , LOLLI, Marco
IPC: C07D295/185 , C07D295/145 , C07C237/08 , C07C237/10 , C07C237/06 , A61K49/00
CPC classification number: C07D295/185 , A61K49/06 , C07C237/06 , C07C237/08 , C07C237/10 , C07D295/15
Abstract: This invention refers to new compounds of formula (I) endowed with a chelating property for paramagnetic bi- and trivalent metal ions, their chelates with said metal ions and their use as contrast agents in magnetic resonance imaging (MRI).
